(57) The present invention relates to a compound for use in labeling a protease having
the formula (II):
wherein D comprises a benzoindole dye; L1 is a linker; AA1 is an amino acid side chain; U is O, NH, or S; R1 is alkyl, alkenyl, alkynyl, aryl, aralkyl, heteroaryl, heteroaralkyl, cycloalkyl,
cycloalkenyl, cycloalkylalkyl, heterocyclyl, heterocyclylalkyl, or a protecting group,
and is optionally substituted with 1 to 3 A groups; each A is independently alkyl,
alkenyl, alkynyl, alkoxy, alkanoyl, alkylamino, aryl, aryloxy, arylamino, aralkyl,
aralkoxy, aralkanoyl, aralkamino, heteroaryl, heteroaryloxy, heteroarylamino, heteroaralkyl,
heteroaralkoxy, heteroaralkanoyl, heteroaralkamino, cycloalkyl, cycloalkenyl, cycloalkylalkyl,
cycloalkoxy, cycloalkanoyl, cycloalkamino, heterocyclyl, heterocyclyloxy, heterocyclylamino,
heterocyclylalkyl, heterocyclylalkoxy, heterocyclylalkanoyl, heterocyclylalkamino,
hydroxyl, thio, amino, alkanoylamino, aroylamino, aralkanoylamino, alkylcarboxy, carbonate,
carbamate, guanidinyl, urea, halo, trihalomethyl, cyano, nitro, phosphoryl, sulfonyl,
sulfonamido, or azido, L3 is a linker; and Q comprises a quencher, and wherein the benzoindole dye has the
structure:
wherein o is an integer from 1 to 4; R2 is a C2-C8 alkyl group, optionally substituted with a sulfonate or carbonate; each R3 is independently a C1-C6 alkyl group; and L4 is an optionally substituted alkyl linker, wherein each carbon atom is optionally
replaced with a heteroatom.
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